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Molecules. 2010 Nov 3;15(11):7871-83. doi: 10.3390/molecules15117871.

Synthesis and tumor cytotoxicity of novel amide derivatives of β-hederin.

Author information

1
Key Laboratory of Structure-Based Drug Design and Discovery (Ministry of Education), Shenyang Pharmaceutical University, Shenyang 110016, China. ly_99@sina.com

Abstract

Thirteen novel triterpenoid saponins, designed as amide derivatives of the natural cytotoxic saponin β-hederin, were synthesized by a stepwise glycosylation strategy. The in vitro cytotoxic activity of these compounds was evaluated against five different tumor cell lines. Most of the evaluated compounds showed effective inhibitory activity against at least one tumor cell line at micromolar concentrations. The preliminary structure-activity relationships (SAR) indicate that mide derivatization at C-28 resulted in highly cytotoxic derivatives on specific tumor cell lines, and also resulted in an increase in the antitumor selectivity of β-hederin. 

PMID:
21060295
DOI:
10.3390/molecules15117871
[Indexed for MEDLINE]
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